TABLE 5.
Anti-HIV and anti-HCV activities of nucleosides 20–23
| Anti-HIV-1 activity in human PBM cells and cytotoxicity in | Anti-HCV activity and toxicity in replicon assay Huh7 cells | |||||||
|---|---|---|---|---|---|---|---|---|
| CC50(μM) | ||||||||
| Compound | EC50 (μM) | EC90 (μM) | PBM | CEM | Vero | EC50 (μM) | EC90 (μM) | CC50b (μM) |
| 20 | 0.72 | 10.3 | >100 | >100 | >100 | >10 | >10 | >10 |
| 21 | 5.6 | >100 | >100 | >100 | >100 | >10 | >10 | >10 |
| 22 | 14.1 | 46.3 | 13.6 | 70.2 | >100 | >10 | >10 | >10 |
| 23 | 60.1 | >100 | 9.4 | >100 | >100 | >10 | >10 | >10 |
| 2′-β-FddAa | 4.4 | — | >100 | — | — | — | — | — |
| AZTc | 0.0026 | 0.010 | >100 | 14.3 | 56.0 | — | — | — |
| 2-C-Me-Cc | — | — | — | — | — | 1.3 | 5.4 | >10 |
a
The anti-HIV activity of lodenosine (2′-β-FddA) 1 in PBM cells was taken from literature [23] and presented for comparison.
b
Toxicity in Huch-7 Replicon cells.
c
AZT and 2′-C-Me C were used as positive controls for the HIV and HCV assays.